First GPR119 PET Imaging Ligand: Synthesis, Radiochemistry, and Preliminary Evaluations.

ABSTRACT: G-protein-coupled receptor 119 (GPR119) has emerged as a promising target for treating type 2 diabetes mellitus. Activating GPR119 improves glucose homeostasis, while suppressing appetite and weight gain. Measuring GPR119 levels in vivo could significantly advance GPR119-based drug development strategies including target engagement, occupancy, and distribution studies. To date, no positron emission tomography (PET) ligands are available to image GPR119. In this paper, we report the synthesis, radiolabeling, and preliminary biological evaluations of a novel PET radiotracer [¹⁸F]KSS3 to image GPR119. PET imaging will provide information on GPR119 changes with diabetic glycemic loads and the efficacy of GPR119 agonists as antidiabetic drugs. Our results demonstrate [^18<

SUBMITTER: Bansode AH 

PROVIDER: S-EPMC10999001 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature